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Assay Detail

CHEMBL763564

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.
Brown PJ, Winegar DA, Plunket KD, Moore LB, Lewis MC, Wilson JG, Sundseth SS, Koble CS, Wu Z, Chapman JM, Lehmann JM, Kliewer SA, Willson TM.
J Med Chem (1999) 42 : 3785 -3788
PubMed 10508427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.69 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278590 GSK-9578 1 7.30
CHEMBL125230 1 6.82
CHEMBL340011 1 6.39
CHEMBL124842 1 6.10
CHEMBL124079 1 5.85
CHEMBL981 FENOFIBRIC ACID 4.0 1 4.52
CHEMBL264374 BEZAFIBRATE 3.0 1 4.30
CHEMBL683 CLOFIBRIC ACID 2.0 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278590 GSK-9578 EC50 = 50.0 nM 7.30
CHEMBL125230 EC50 = 150.0 nM 6.82
CHEMBL340011 EC50 = 410.0 nM 6.39
CHEMBL124842 EC50 = 790.0 nM 6.10
CHEMBL124079 EC50 = 1400.0 nM 5.85
CHEMBL981 FENOFIBRIC ACID EC50 = 30000.0 nM 4.52
CHEMBL264374 BEZAFIBRATE EC50 = 50000.0 nM 4.30
CHEMBL683 CLOFIBRIC ACID EC50 = 55000.0 nM 4.26